期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 32, 期 1, 页码 1216-1228出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1368503
关键词
Diabetes; flavonoids; alpha-glucosidase inhibition; in vitro; in silico
资金
- Fundacao para a Ciencia e Tecnologia
- European Union funds [Fundo Europeu de Desenvolvimento Regional (FEDER)] under the program PT2020 [PT2020 UID/MULTI/04378/2013 - POCI/01/0145/FEDER/007728, NORTE-01-0145-FEDER-000024]
- European Union funds [Fundo Europeu de Desenvolvimento Regional (FEDER)] under Programa Operacional Competitividade e Internacionalizacao (COMPETE)
- FCT [SFRH/BD/116005/2016, PTDC/QEQ-QAN/1742/2014 - POCI-01-0145-FEDER-016530]
- Fundo Social Europeu (FSE)
- Ministerio da Ciencia, Tecnologia e Ensino Superior (MCTES)
- Daniela Ribeiro acknowledges FEDER, through COMPETE
- Ministerio da Educacao e Ciencia (FCT/MEC)]
alpha-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia ( PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of alpha-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A-and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC50 much lower than the one found for the most widely prescribed alpha-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.
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